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GNE-6640 is a selective, non-covalently bound inhibitor of ubiquitin-specific peptidase 7 (USP7) with IC50 values of 0.75 μM, 0.43 μM, 20.3 μM and 0.23 μM for USP7 full-length, USP7 catalytic domain, USP43 full-length and Ub-MDM2, respectively. cytotoxicity of chemotherapeutic agents and targeted compounds, including PIM kinase inhibitors.
| Molecular Weight | 330.38 |
| Formula | C20H18N4O |
| CAS Number | 2009273-67-8 |
| Solubility (25°C) | DMSO : 5 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[1] Lorna Kategaya, et al. Nature. USP7 small-molecule inhibitors interfere with ubiquitin binding
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